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Literature summary for 2.3.1.286 extracted from

  • Maurer, B.; Rumpf, T.; Scharfe, M.; Stolfa, D.A.; Schmitt, M.L.; He, W.; Verdin, E.; Sippl, W.; Jung, M.
    Inhibitors of the NAD(+)-dependent protein desuccinylase and demalonylase Sirt5 (2012), ACS Med. Chem. Lett., 3, 1050-1053.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.3.1.286

Inhibitors

Inhibitors Comment Organism Structure
(5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 10% inhibition at 0.05 mM Homo sapiens
(5E)-5-(1H-indol-3-ylmethylidene)-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 17% inhibition at 0.05 mM; 20% inhibition at 0.05 mM Homo sapiens
(5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 13% inhibition at 0.05 mM Homo sapiens
(5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 25% inhibition at 0.05 mM Homo sapiens
(5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 22% inhibition at 0.05 mM Homo sapiens
(5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 41% inhibition at 0.05 mM Homo sapiens
2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate i.e. Ro 31-8220; i.e. Ro 31-8220; i.e. Ro 31-8220 Homo sapiens
5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 14% inhibition at 0.05 mM Homo sapiens
5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 20% inhibition at 0.05 mM Homo sapiens
5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 13% inhibition at 0.05 mM Homo sapiens
5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 30% inhibition at 0.05 mM Homo sapiens
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide i.e. EX-527; i.e. EX-527; i.e. EX-527 Homo sapiens
cambinol
-
 Homo sapiens
additional information no inhibition at 0.05 mM: (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition at 0.05 mM: (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220 Homo sapiens
nicotinamide
-
 Homo sapiens
sirtinol 24% inhibition at 0.05 mM Homo sapiens
suramin
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8IXJ6
-
-
Homo sapiens Q96EB6
-
-
Homo sapiens Q9NTG7
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
NAD+ + N2-benzyloxycarbonyl-N6-succinyl-L-lysine-7-amido-4-methylcoumarin i.e. 3-[(5-[[(benzyloxy)carbonyl]amino]-5-[(4-methyl-2-oxo-2H-chromen-7-yl)carbamoyl]pentyl)carbamoyl]-propanoic acid Homo sapiens nicotinamide + N2-benzyloxycarbonyl-L-lysine-7-amido-4-methylcoumarin + 2'-O-succinyl-ADP-ribose
-
 ?
NAD+ + N2-benzyloxycarbonyl-N6-succinyl-L-lysine-7-amido-4-methylcoumarin i.e. 3-[(5-[[(benzyloxy)carbonyl]amino]-5-[(4-methyl-2-oxo-2H-chromen-7-yl)carbamoyl]pentyl)carbamoyl]-propanoic acid Homo sapiens nicotinamide + N2-benzyloxycarbonyl-L-lysine-7-amido-4-methylcoumarin + 2'-O-succinyl-ADP ribose
-
 ?

Synonyms

Synonyms Comment Organism
SIRT1
-
 Homo sapiens
SIRT2
-
 Homo sapiens
SIRT3
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001 0.001 pH 8.0, 37°C Homo sapiens 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
0.0003 0.0026 pH 8.0, 37°C Homo sapiens suramin
0.0008
-
 pH 8.0, 37°C Homo sapiens 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
0.0011 0.02 pH 8.0, 37°C Homo sapiens suramin
0.0012 0.1 pH 8.0, 37°C Homo sapiens nicotinamide
0.0034
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0035
-
 pH 8.0, 37°C Homo sapiens 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
0.0037
-
 pH 8.0, 37°C Homo sapiens 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
0.0075
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0087
-
 pH 8.0, 37°C Homo sapiens 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0097
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0098
-
 pH 8.0, 37°C Homo sapiens 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.01
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0104
-
 pH 8.0, 37°C Homo sapiens 5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0117
-
 pH 8.0, 37°C Homo sapiens 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0144
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0147
-
 pH 8.0, 37°C Homo sapiens 5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.02 0.033 pH 8.0, 37°C Homo sapiens 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
0.0203
-
 pH 8.0, 37°C Homo sapiens 5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0293
-
 pH 8.0, 37°C Homo sapiens 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.03
-
 pH 8.0, 37°C Homo sapiens nicotinamide
0.0303
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.037 0.131 pH 8.0, 37°C Homo sapiens sirtinol
0.038 0.058 pH 8.0, 37°C Homo sapiens sirtinol
0.0403
-
 pH 8.0, 37°C Homo sapiens 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0433
-
 pH 8.0, 37°C Homo sapiens 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.0464
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
0.049
-
 pH 8.0, 37°C Homo sapiens 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
0.05 0.1 pH 8.0, 37°C Homo sapiens nicotinamide
0.056
-
 pH 8.0, 37°C Homo sapiens cambinol
0.059
-
 pH 8.0, 37°C Homo sapiens cambinol
0.116
-
 pH 8.0, 37°C Homo sapiens 5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione